An aporphine alkaloid from Nelumbo nucifera as an acetylcholinesterase inhibitor and the primary investigation for structure–activity correlations
2011; Taylor & Francis; Volume: 26; Issue: 5 Linguagem: Inglês
10.1080/14786419.2010.487188
ISSN1478-6427
AutoresZhong‐Duo Yang, Xu Zhang, Juan Du, Zhao-jian Ma, Feng Guo, Shuo Li, Xiaojun Yao,
Tópico(s)Cholinesterase and Neurodegenerative Diseases
ResumoN-methylasimilobine (1), a new-found strong acetylcholinesterase (AChE) inhibitor, along with two weakly active aporphine alkaloids, nuciferine (2) and nornuciferine (3) were separated from Nelumbo nucifera. N-methylasimilobine (1) inhibited 50% of AChE activity at the concentrations of 1.5 ± 0.2 µg mL(-1) when the standard IC(50) value of Physostigmine was 0.013 ± 0.002 µg mL(-1). The mode of AChE inhibition by 1 was reversible and non-competitive. In addition, molecular modelling was performed to explore the binding mode of inhibitor 1 at the active site of AChE.
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